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AMBRISENTAN
Generic Name: AMBRISENTAN
ABSTRACT -
Ambrisentan is an orally active selective endothelin receptor type A antagonist used in the treatment of pulmonary arterial hypertension (PAH, WHO Group 1). By blocking endothelin-mediated vasoconstriction and vascular smooth-muscle proliferation, it helps reduce pulmonary vascular resistance and improve exercise capacity.
It is available as prescription oral tablets and is used alone or, in selected patients, with other PAH therapies such as tadalafil under specialist supervision.
DOSAGE -
Dosage should be determined only by a qualified healthcare professional experienced in PAH treatment.
Typical adult initiation is 5 mg orally once daily.
The dose may be increased to 10 mg once daily as needed and tolerated.
When co-administered with cyclosporine, the ambrisentan dose should generally be limited to 5 mg once daily.
Tablets should be swallowed whole and not split, crushed, or chewed unless directed by the prescriber.
SIDE EFFECTS–
Common or clinically important side effects include:
- Peripheral edema or fluid retention
- Nasal congestion or sinusitis
- Flushing
- Headache
- Palpitations
- Anemia or decreased hemoglobin
- Nausea
- Elevated liver enzymes or liver-related symptoms
- Shortness of breath or worsening heart failure symptoms in susceptible patients
ALLRGIC REACTIONS–
Hypersensitivity to ambrisentan or tablet excipients is possible. Patients with a previous allergic reaction to ambrisentan should not use it unless a specialist determines otherwise.
Symptoms may include:
- Skin rash or hives
- Itching or swelling of the face, lips, tongue, or throat
- Difficulty breathing or chest tightness
- Severe dizziness or fainting
- Unexpected widespread redness, blistering, or peeling skin
Important: Patients who develop an allergic reaction to Ambrisentan should seek immediate medical attention and inform all future healthcare providers of the allergy.
DRUG INTERACTIONS–
Ambrisentan may interact with certain medicines or substances. Caution is needed with:
- Cyclosporine, which can increase ambrisentan exposure; dose limitation is recommended
- Other PAH medicines, including tadalafil, which may require specialist dose adjustment
- Strong transporter or metabolic enzyme inhibitors or inducers when clinically relevant
- Medicines that may worsen fluid retention or edema
- Alcohol if dizziness, hypotension, or liver-related concerns occur
Patients should inform healthcare providers about all prescription medicines, over-the-counter medicines, herbal products, and supplements they are using.
PREAUTIONS–
Pregnancy testing and strict contraception are required for patients who can become pregnant.
- Monitor for edema, anemia, worsening dyspnea, and signs of heart failure.
- Check hemoglobin/hematocrit before and during therapy as clinically indicated.
- Use is not recommended in moderate or severe hepatic impairment.
- Use only for PAH patients under specialist supervision.
WARNINGS –
- Contraindicated in pregnancy because of embryo-fetal toxicity.
- Do not start therapy in patients who are pregnant or planning pregnancy.
- Seek urgent care for severe shortness of breath, rapid weight gain, fainting, or signs of liver injury.
- Do not use for idiopathic pulmonary fibrosis unless specifically prescribed for an approved indication.
- Keep out of reach of children.
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